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A structure-activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity.

ABSTRACT: We report the synthesis, cytotoxicity, and phenotypic analysis of oxazole and thiazole containing fragments. Evaluating the optimal size and heterocycle for growth inhibition and apoptosis showed that activity required at least two thiazoles sequentially connected. This is the first detailed comparison of biological activity between multi-heterocyclic containing fragments.

SUBMITTER: Kim SJ

PROVIDER: S-EPMC3601786 | biostudies-literature | 2013 Feb

REPOSITORIES: biostudies-literature

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A structure-activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity.

Kim Seong Jong SJ Lin Chun Chieh CC Pan Chung-Mao CM Rananaware Dimple P DP Ramsey Deborah M DM McAlpine Shelli R SR

MedChemComm 20121129 2

We report the synthesis, cytotoxicity, and phenotypic analysis of oxazole and thiazole containing fragments. Evaluating the optimal size and heterocycle for growth inhibition and apoptosis showed that activity required at least two thiazoles sequentially connected. This is the first detailed comparison of biological activity between multi-heterocyclic containing fragments. ...[more]

PMID: 23524379

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